Jeffamine® Core PAMAM Dendrimers as Solubility Enhancer of Carvedilol

Abstract

The aim of this study was to investigate the effect of Jeffamine® core poly(amidoamine) PAMAM dendrimers (JCPDs) on the aqueous solubility of carvedilol (CAR), a Biopharmaceutical Classification System (BCS) Class II drug, and a nonselective beta-adrenegenic blocking agent with alpha 1-blocking activity. The aqueous solubility of CAR was measured in the presence of JCPDs at room temperature in phosphate-buffered saline using traditional rotating bottle technique. Results obtained from the phase solubility studies revealed that the molar aqueous solubility of CAR increased significantly with a proportional increase in the concentration of fourth-generation JCPD, P4.NH2. Likewise, the encapsulation efficiency of JCPD, P4.NH2 improved as its concentration increased and the highest capacity was observed to be 60.75%. Furthermore, the drug binding constant of P4.NH2 (11177.31 ± 0.15 M-1) was found to be fifty times higher than that of β-cyclodextrin (227 M-1), which is the most common studied solubility enhancer excipient for CAR drug. Overall, it can be concluded that PAMAMs, used for the first time in this study as the successful solubility enhancer of CAR, might be helpful and good candidates for the development of various formulations in the future studies.